Desyrel

Trazodone (Desyrel®, Trittico®, Thombran®, Trialodine®) is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. The manufacturer claims that the antidepressant activity becomes evident in the first week of therapy. Trazodone has less prominent anticholinergic (dry mouth, constipation, tachycardia) and adrenolytic (hypotension, male sexual problems) side effects than most tricyclic antidepressants. The incidence of nausea and vomiting observed with Trazodone is relatively low compared to SSRIs. more...

Mechanism of action

Trazodone is a serotonin reuptake inhibitor and is also a 5-HT₂ receptor antagonist. However, in contrast to the selective serotonin reuptake inhibitors such as fluoxetine (Prozac®), trazodone's antidepressant effects may be due to the antagonism of 5-HT₂ receptors (PMID 1365657).

Pharmacokinetics

Trazodone is well absorbed after oral administration with mean peak plasma levels obtained at approximately 1 hour after ingestion. Absorption is somewhat delayed and enhanced by food. The mean plasma elimination half-life is biphasic: the first phase's half-life is 3-6 hours, and the following phase's half-life is 5-9 hours. The drug is extensively metabolized with 3 or 4 major metabolites having been identified in man. Approximately 70-75% of C¹⁴-labelled trazodone was found to be excreted in the urine within 72 hours (PMID 1037253). Trazodone is highly protein-bound.

Uses

• Depression with or without anxiety
• Chronic Insomnia (in some countries, this is an off-label use)

Contraindications

• Known hypersensitivity to trazodone
• Use in patients below 18 years of age

Precautions

Trazodone is metabolised by CYP3A4, a liver enzyme (PMID 9616194). Inhibition of this enzyme by various other substances may delay its degradation, leading to high blood levels of trazodone. CYP3A4 may be inhibited by many other medications, herbs, and foods, and as such, trazodone may interact with these substances. One drug-food interaction is grapefruit juice. Drinking grapefruit juice is discouraged in patients taking trazodone.

One glass of grapefruit juice once in a while is not likely to have this effect on most people, but drinking large amounts, or drinking it regularly is proven to.

The possibility of suicide in depressed patients remains during treatment and until significant remission occurs. Therefore, the number of tablets prescribed at any one time should take into account this possibility, and patients with suicide ideation should never have access to large quantities of trazodone.

Episodes of complex partial seizures have been reported in a small number of patients. The majority of these patients were already receiving anticonvulsant therapy for a previously diagnosed seizure disorder.

Pregnancy and Lactation

• Pregnancy : Sufficient data in humans is lacking. The use should be justified by the severity of the condition to be treated.

• Lactation : Sufficient data in humans is also lacking. Additionally, trazodone may be found in the maternal milk in significant concentrations. The use in breastfeeding women should be carefully weighed against possible risks.

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